Research on antibacterial and antifungal agents. XIII. Synthesis and antimicrobial activity of 1-arylmethyl-4-aryl-1H-pyrrole-3-carboxylic acids.
Several 1-arylmethyl-4-aryl-1H-pyrrole-3-carboxylic acid derivatives have been synthetized and tested as antifungal and antibacterial agents. Reaction between tosylmethylisocyanide (TosMIC) and beta-arylacrylic esters under basic conditions furnished 4-aryl-1H-pyrrole-3-carboxylic esters, which were then benzylated at 1 position. Alkaline hydrolysis of ethyl 1-arylmethyl-4-aryl-1H-pyrrole-3-carboxylates afforded the title compounds. All tested derivatives were found to be inactive as antifungal agents. Some of them showed appreciable antibacterial activities against Staphylococcus spp.
Massa
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Dipartimento di Studi Farmaceutici, Università di Roma La Sapienza, Italy.
Di Santo
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R
Mai
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A
Botta
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M
Artico
M
M
Panico
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S
Simonetti
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G
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000138:chemical synthesis*; D000935:Antifungal Agents / Q000138:chemical synthesis*; D001419:Bacteria / Q000187:drug effects; D002175:Candida / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013055:Spectrophotometry, Infrared
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000935:Antifungal Agents; D011758:Pyrroles